Established in 2010, the target company focuses on small molecule medicines which are used for cancer and immune system disorders. It has built a rich pipeline based on proprietary discovery platforms, TALENTTM, FD2TM and PD2TM.
The company is looking for partners to develop and commercialize the asset globally or regionally.
Asset: Asset 1–CXCR4 antagonist; Asset 2–FGFR and VEGFR dual inhibitor; Asset 2–ALK inhibitor; Asset 4–CDK Inhibitor
Status: Ongoing ph1 (Asset 1, 2 & 3); IND-Enabling (Asset 4)
Indications: Solid tumors and hematopoietic malignancies
Asset 1 Highlights:
- The first oral CXCR4 antagonist medication. No oral CXCR4 antagonist is commercially available yet.
- Clean GPCR selectivity profile. 1μM Asset1 results in 113% inhibition of CXCR4 without any significant effect (EC50/IC50>10μM) on 47 safety-relevant targets.
- Potent hematopoietic stem cell mobilizing effect is observed in animal models. In beagle dogs, the amount of CD34+ cells and whole blood WBC are in a dose-dependent manner and increased significantly at all the low, medium and high concentration groups.l Synergistic with multiple drugs. The combined administration of Asset 1 and G-CSF has a better effect on mouse hematopoietic stem cell mobilization than G-CSF alone.
Asset 2 Highlights:
- Selectively against most other kinases. The target kinase inhibitory activity against FGFR and VEGFR is 2-8 times higher than ODM203.
- Better oral bioavailability (59% in mice, 34% in rats, 57% in dogs) than ODM203 (45% in mice, 10% in rats, 51% in dogs)
- The synergistic effect of inhibiting both FGFR and VEGFR has been confirmed in animal model studies.
- The product shows excellent PK, especially the AUC is 3-fold higher than ODM203. It is predicted that the product just needs half a dose of the ODM203 to achieve the same therapeutic effect in human.
Asset 3 Highlights:
- 2-10 times inhibitory activity than alectinib against ALK.
- Significantly inhibit tumor growth in female Nude Mice bearing NCI-H3122 NSCLC Xenograft. The relative tumor growth rates (T/C) of Asset3 is 2.75% (P < 0.001), versus 47.80% of alectinib compare to vehicle.
- Potent activity against RET kinase and RET-driven tumor cell lines, and IC50 is 150 times lower than that of alectinib.
Asset 4 Highlights:
- Superior efficacy than Abemaciclib and Palbociclib at the same dosage level in AML and MCL mouse orthotopic models. The proportion of hCD4+ cells in bone marrow and blood was significantly reduced as well as the body weight coefficient of spleen in a dose-dependent manner.
- nM-level cytostatic activity in hematological cell lines.
- The product will focus on mutations in acute myeloid leukemia, and there is no CDK inhibitor approved for commercialization for hematological disorders yet.